EA200701239A1 - 18-METHYL-9-NOR-17-PREGN-4-EN-21,17-CARBOLAKTONY, AND ALSO THE MEDICINAL PREPARATIONS THERE ARE CONTAINED - Google Patents

18-METHYL-9-NOR-17-PREGN-4-EN-21,17-CARBOLAKTONY, AND ALSO THE MEDICINAL PREPARATIONS THERE ARE CONTAINED

Info

Publication number
EA200701239A1
EA200701239A1 EA200701239A EA200701239A EA200701239A1 EA 200701239 A1 EA200701239 A1 EA 200701239A1 EA 200701239 A EA200701239 A EA 200701239A EA 200701239 A EA200701239 A EA 200701239A EA 200701239 A1 EA200701239 A1 EA 200701239A1
Authority
EA
Eurasian Patent Office
Prior art keywords
methyl
atom
hydrogen
carbon atoms
branched chain
Prior art date
Application number
EA200701239A
Other languages
Russian (ru)
Other versions
EA014325B1 (en
Inventor
Рольф Больманн
Дитер Биттлер
Германн Кюнцер
Петер Эсперлинг
Ханс Петер Мун
Карл-Генрих Фритцемайер
Ульрике Фурманн
Катя Прелле
Борден, (ранее Курц) Штеффен
Original Assignee
Байер Шеринг Фарма Акциенгезельшафт
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=36087369&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA200701239(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Байер Шеринг Фарма Акциенгезельшафт filed Critical Байер Шеринг Фарма Акциенгезельшафт
Publication of EA200701239A1 publication Critical patent/EA200701239A1/en
Publication of EA014325B1 publication Critical patent/EA014325B1/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A61K31/585—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18—Feminine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/34—Gestagens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J53/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
    • C07J53/002—Carbocyclic rings fused
    • C07J53/004—3 membered carbocyclic rings
    • C07J53/008—3 membered carbocyclic rings in position 15/16

Abstract

Настоящее изобретение касается новых 18-метил-19-нор-17-прегн-4-ен-21,17-карболактонов общей формулы Iв которой Z представляет собой атом кислорода, два атома водорода, группировку =NOR или =NNHSOR, причем R означает атом водорода или алкильную группу с прямой или разветвленной цепью, содержащей от 1 до 4 или от 3 до 4 атомов углерода, Rозначает атом водорода, атом галогена, метильную или трифторметильную группу, Rи/или Rможет находиться в α или β и независимо друг от друга означает алкильную группу с прямой или разветвленной цепью, содержащей от 1 до 4 или от 3 до 4 атомов углерода, или Rозначает атом водорода и Rозначает расположенную α или β алкильную группу с прямой или разветвленной цепью, содержащей от 1 до 4 или от 3 до 4 атомов углерода, или Rи Rкаждый означает один атом водорода, или Rи Rвместе означают расположенную α или β метиленовую группу или дополнительную связь. Новые соединения обладают гестагенным и антиминералокортикоидным действием и являются пригодными для получения лекарственных препаратов, например, для пероральной контрацепции и для лечения пре-, пери- и постменопаузальных расстройств.The present invention relates to new 18-methyl-19-nor-17-pregn-4-ene-21,17-carbolactones of the general formula I in which Z represents an oxygen atom, two hydrogen atoms, a group = NOR or = NNHSOR, wherein R is an atom hydrogen or a straight or branched chain alkyl group containing from 1 to 4 or from 3 to 4 carbon atoms, R represents a hydrogen atom, a halogen atom, a methyl or trifluoromethyl group, R and / or R may be in α or β and independently from each other means straight or branched chain alkyl group containing from 1 to 4 or from 3 up to 4 carbon atoms, or R represents a hydrogen atom and R denotes a straight or branched chain located α or β alkyl group containing from 1 to 4 or from 3 to 4 carbon atoms, or R and R each mean one hydrogen atom, or R and R together mean a located α or β methylene group or an additional bond. The new compounds have a progestational and antimineralocorticoid effect and are suitable for the manufacture of medications, for example, for oral contraception and for the treatment of pre-, peri- and postmenopausal disorders.

EA200701239A 2004-12-30 2005-12-30 18-methyl-19-nor-17-pregn-4-en-21,17-carbolactones and pharmaceutical preparations comprising the same EA014325B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102004063864A DE102004063864A1 (en) 2004-12-30 2004-12-30 18-methyl-19-nor-17-pregn-4-en21,17-carbolactones, as well as pharmaceutical compositions containing them
PCT/EP2005/014205 WO2006072467A1 (en) 2004-12-30 2005-12-30 18-methyl-19-nor-17-pregn-4-en-21,17-carbolactones and pharmaceutical preparations comprising the same

Publications (2)

Publication Number Publication Date
EA200701239A1 true EA200701239A1 (en) 2007-12-28
EA014325B1 EA014325B1 (en) 2010-10-29

Family

ID=36087369

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200701239A EA014325B1 (en) 2004-12-30 2005-12-30 18-methyl-19-nor-17-pregn-4-en-21,17-carbolactones and pharmaceutical preparations comprising the same

Country Status (33)

Country Link
US (1) US20090029953A1 (en)
EP (1) EP1831240B8 (en)
JP (1) JP5043681B2 (en)
KR (1) KR20070093443A (en)
CN (1) CN101128476B (en)
AR (1) AR052657A1 (en)
AU (1) AU2005324055A1 (en)
BR (1) BRPI0518533A2 (en)
CA (1) CA2594171C (en)
CR (1) CR9223A (en)
CY (1) CY1109498T1 (en)
DE (2) DE102004063864A1 (en)
DK (1) DK1831240T3 (en)
EA (1) EA014325B1 (en)
ES (1) ES2331322T3 (en)
GT (1) GT200500394A (en)
HK (1) HK1112627A1 (en)
IL (1) IL184288A (en)
MX (1) MX2007008074A (en)
MY (1) MY145904A (en)
NO (1) NO20073257L (en)
NZ (1) NZ556150A (en)
PA (1) PA8658401A1 (en)
PE (2) PE20060853A1 (en)
PL (1) PL1831240T3 (en)
PT (1) PT1831240E (en)
RS (1) RS51128B (en)
SI (1) SI1831240T1 (en)
TW (1) TW200635942A (en)
UA (1) UA90496C2 (en)
UY (1) UY29320A1 (en)
WO (1) WO2006072467A1 (en)
ZA (1) ZA200706254B (en)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102006030416A1 (en) * 2006-06-29 2008-01-03 Bayer Schering Pharma Ag 18-methyl-19-nor-androst-4-ene-17,17-spiroethers (18-methyl-19-nor-20-spirox-4-en-3-ones) and pharmaceutical compositions containing them
DE102007027636A1 (en) * 2007-06-12 2008-12-18 Bayer Schering Pharma Aktiengesellschaft 17β-Cyano-18α-homo-19-nor-androst-4-ene derivative, its use and the derivative-containing drug
DE102007027637A1 (en) 2007-06-12 2008-12-18 Bayer Schering Pharma Aktiengesellschaft 17β-cyano-19-nor-androst-4-ene derivative, its use and the derivative-containing drug
DE102007027635A1 (en) * 2007-06-12 2008-12-18 Bayer Schering Pharma Aktiengesellschaft 17β-cyano-19-androst-4-ene derivative, its use and the derivative-containing drug
DE102007063501A1 (en) * 2007-12-29 2009-07-02 Bayer Schering Pharma Aktiengesellschaft 15, 16-methylene-17-hydroxy-19-nor-21-carboxylic acid steroid y-lactone derivative, its use and the derivative-containing drug
DE102007063500A1 (en) * 2007-12-29 2009-07-02 Bayer Schering Pharma Aktiengesellschaft 17- (1'-Propenyl) -17-3'-oxidoestra-4-en-3-one derivative, its use and the derivative-containing drug
DE102007063503A1 (en) * 2007-12-29 2009-07-02 Bayer Schering Pharma Aktiengesellschaft 17-hydroxy-19-nor-21-carboxylic acid steroid y-lactone derivative, its use and the derivative-containing drug
DE102007063495A1 (en) * 2007-12-29 2009-09-17 Bayer Schering Pharma Aktiengesellschaft 19-nor-steroid derivatives having a 15α, 16α-methylene group and a saturated 17,17-spirolactone ring, their use and medicaments containing these derivatives
DE102007063498A1 (en) 2007-12-29 2009-07-02 Bayer Schering Pharma Aktiengesellschaft 15,16-methylene-steroid-17,17-lactol derivative, its use and the derivative-containing drug
DE102007063496A1 (en) * 2007-12-29 2009-07-02 Bayer Schering Pharma Aktiengesellschaft 15,16-Methylene-17- (1'-propenyl) -17-3'-oxidoestra-4-en-3-one derivative, its use and the derivative-containing drug
DE102007063499A1 (en) 2007-12-29 2009-07-02 Bayer Schering Pharma Aktiengesellschaft Steroid 17,17-lactol derivative, its use and the derivative containing drug
US7960368B2 (en) * 2008-03-05 2011-06-14 Everstra, Inc. Bismethylene-17A carbolactones and related uses
DE102008026793A1 (en) 2008-06-02 2009-12-03 Bayer Schering Pharma Aktiengesellschaft C-ring-substituted pregn-4-ene-21,17-carbolactones, as well as pharmaceutical compositions containing them
CN101623287B (en) * 2008-07-07 2012-02-08 天津金耀集团有限公司 Novel drospirenone analogue medicinal composition for treating menopausal syndrome
US8222237B2 (en) * 2008-11-25 2012-07-17 Evestra, Inc. Progestational 3-(6,6-ethylene-17B-hydroxy-3-oxo-17A-pregna-4-ene-17A-yl)propionic acid G-lactones
WO2010066349A1 (en) * 2008-12-12 2010-06-17 Bayer Schering Pharma Aktiengesellschaft Use of 17beta-cyano-19-androst-4-ene derivatives for manufacturing a medicament in a sustained-release form for parenteral use, and sustained-release medicament containing 17beta-cyano-19-androst-4-ene derivatives for parenteral use
WO2010066355A1 (en) * 2008-12-12 2010-06-17 Bayer Schering Pharma Aktiengesellschaft USE OF 17β-CYANO-19-NOR-ANDROST-4-ENE DERIVATIVES FOR MANUFACTURING A MEDICAMENT IN A SUSTAINED-RELEASE FORM FOR PARENTERAL USE, AND SUSTAINED-RELEASE MEDICAMENT CONTAINING 17β-CYANO-19-NOR-ANDROST-4-ENE DERIVATIVES FOR PARENTERAL USE
WO2010066354A1 (en) * 2008-12-12 2010-06-17 Bayer Schering Pharma Aktiengesellschaft USE OF 17β-CYANO-18A-HOMO-19-NOR-ANDROST-4-ENE DERIVATIVES FOR MANUFACTURING A MEDICAMENT IN A SUSTAINED-RELEASE FORM FOR PARENTERAL USE, AND SUSTAINED-RELEASE MEDICAMENT CONTAINING 17β-CYANO-18A-HOMO-19-NOR-ANDROST-4-ENE DERIVATIVES FOR PARENTERAL USE
WO2012059594A1 (en) 2010-11-04 2012-05-10 Bayer Pharma Aktiengesellschaft Mineralcorticoid receptor antagonists for the treatment of corticoid-induced obesity

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US3959322A (en) * 1960-09-22 1976-05-25 Herchel Smith Synthesis of 13-alkyl-gon-4-ones
DE3022337A1 (en) * 1980-06-11 1982-01-07 Schering Ag Berlin Und Bergkamen, 1000 Berlin Compsns. for contraception or treatment of gynaecological disorders - contg. 6 beta, 7 beta; 15 delta, 16 beta-di:methylene-3-oxo-4-androstene-17(beta-1')-spiro-5'-per:hyd- ro-furan-2'-one
DE3402329A1 (en) * 1984-01-20 1985-08-01 Schering AG, 1000 Berlin und 4709 Bergkamen 6,6-ETHYLENE-15,16-METHYLENE-3-OXO-17 (ALPHA) -PREGN-4-EN-21,17-CARBOLACTONE, METHOD FOR THE PRODUCTION THEREOF AND PHARMACEUTICAL PREPARATIONS CONTAINING THEM
FR2739029B1 (en) * 1995-09-21 1997-11-21 Roussel Uclaf NEW THERAPEUTIC APPLICATION OF ANTIMINERALOCORTICOID COMPOUNDS
DE19651000A1 (en) * 1996-12-01 1998-06-04 Schering Ag Oxyiminopregnancarbolactone

Also Published As

Publication number Publication date
CA2594171A1 (en) 2006-07-13
CN101128476A (en) 2008-02-20
EP1831240B1 (en) 2009-07-15
HK1112627A1 (en) 2008-09-12
CY1109498T1 (en) 2014-08-13
EP1831240B8 (en) 2010-02-17
BRPI0518533A2 (en) 2008-11-25
GT200500394A (en) 2006-08-01
UY29320A1 (en) 2006-07-31
CN101128476B (en) 2011-02-09
EA014325B1 (en) 2010-10-29
CR9223A (en) 2007-11-23
DE102004063864A1 (en) 2006-07-13
NZ556150A (en) 2011-02-25
JP5043681B2 (en) 2012-10-10
UA90496C2 (en) 2010-05-11
DE502005007723D1 (en) 2009-08-27
AU2005324055A1 (en) 2006-07-13
PT1831240E (en) 2009-10-22
US20090029953A1 (en) 2009-01-29
WO2006072467A1 (en) 2006-07-13
AR052657A1 (en) 2007-03-28
NO20073257L (en) 2007-08-29
PL1831240T3 (en) 2010-01-29
PE20100736A1 (en) 2010-12-03
TW200635942A (en) 2006-10-16
RS51128B (en) 2010-10-31
PA8658401A1 (en) 2006-08-03
EP1831240A1 (en) 2007-09-12
ES2331322T3 (en) 2009-12-29
PE20060853A1 (en) 2006-09-15
IL184288A (en) 2011-06-30
MX2007008074A (en) 2008-03-10
DK1831240T3 (en) 2009-11-23
SI1831240T1 (en) 2009-12-31
MY145904A (en) 2012-05-15
IL184288A0 (en) 2007-10-31
JP2008526709A (en) 2008-07-24
ZA200706254B (en) 2008-12-31
KR20070093443A (en) 2007-09-18
CA2594171C (en) 2012-10-16

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

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